Camptothecin: Nature’s Potent Topoisomerase Inhibitor for Oncology & Analysis | Supplier & Manufacturer
1. What is Camptothecin?
Camptothecin (CPT) is a pentacyclic quinoline alkaloid initially remoted from the bark/stems of the Chinese language Comfortable Tree (Camptotheca acuminata). It features as a potent topoisomerase I (Topo I) inhibitor, binding to the Topo I-DNA advanced and stopping DNA religation throughout replication. This triggers replication fork collapse, double-strand DNA breaks, ug S-phase selective apoptosis in quickly dividing cells. Its distinctive mechanism underpins its significance in oncology therapeutics ug most cancers biology analysis.
2. Supply, Chemical Properties & Identifiers
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Supply: Panguna nga gikuha gikan sa Camptotheca acuminata bark/seeds. Semi-synthesis from plant precursors is widespread.
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Mga Kinaiya sa Kemikal:
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Ngalan sa Kemikal: (S)-4-Ethyl-4-hydroxy-1H-pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
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Molekular nga mga sangkap: C₂₀H₁₆N₂O₄
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Molekular nga Timbang: 348.36 g/mol
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Panagway: Pale yellow to gentle inexperienced crystalline powder
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Solubility: Lactone ring pH-dependence – Soluble in DMSO, DMF, chloroform (closed lactone kind, energetic); hydrolyzes to inactive carboxylate kind in aqueous pH >7.
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Kalig-on: Mild and pH-sensitive. Requires strict management of lactone ring integrity for bioactivity.
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Panguna nga mga Identifier:
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CAS: 7689-03-4
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Gidaghanon sa EC (EINECS): 231-684-4
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MF: C₂₀H₁₆N₂O₄
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MW: 348.36
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3. Purity, Efficacy, Security & Dosage
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Optimum Product: The “finest” camptothecin options >99% HPLC purity, >95% lactone kind content material (important for exercise), and undetectable contaminants. Shaanxi Zhonghong achieves this by way of proprietary pH-controlled crystallization ug lyophilization.
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Well being Benefits & Functions:
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Anticancer Exercise: Core mechanism: Topo I inhibition → DNA harm → S-phase apoptosis. Foundation for FDA-approved derivatives (Irinotecan, Topotecan) treating colorectal, ovarian, SCLC, cervical cancers.
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Antiviral/Antiparasitic Analysis: Rising exercise towards HIV-1, HSV, Leishmania in preclinical fashions.
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(Be aware: Nattokinase primarily exhibits anticoagulant/thrombolytic results; direct kidney advantages are much less established vs. potential CPT nephrotoxicity issues).
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Dosage & Administration:
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NOT a dietary complement. Used clinically as IV derivatives below strict medical supervision.
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Analysis doses differ (usually 0.1-100 µM sa vitro; mg/kg ranges sa vivo). No secure each day consumption for self-administration exists.
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Important Precautions & Aspect Results:
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Extreme Toxicity: Myelosuppression (neutropenia, thrombocytopenia), extreme diarrhea (cholinergic & delayed), hemorrhagic cystitis, hepatotoxicity.
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Lactone Instability: Speedy hydrolysis to inactive carboxylate at physiological pH reduces efficacy.
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Contraindications: Being pregnant/lactation (teratogenic), pre-existing bone marrow melancholy, energetic infections.
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Pag-atubang sa: Cytotoxic – Requires PPE (gloves, masks, lab coat). Keep away from inhalation/pores and skin contact.
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4. Shaanxi Zhonghong: Your Premier Camptothecin Supply
Shaanxi Zhonghong Investment Technology Co., Ltd. is a cGMP/ISO-certified chief in high-purity plant-derived APIs. With 28+ years in bioactive phytochemistry, we focus on:
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Core Capabilities:
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Siyentipikanhong Excellence: 5 College Joint Labs, 20+ Patents (incl. CPT stabilization tech), Unique Natural Compound Library.
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Slicing-Edge Analytics: HPLC-PDA/ELSD (purity), UPLC-QTOF-MS (impurity profiling), Superconducting FT-NMR (construction ID), ICP-MS (bug-at nga metal), GC-MS/MS (residual solvents). Purity >99%, exceeding USP by 20%.
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Internasyonal nga Pagkab-ot: Naghatag 80+ ka nasod – Pharma, Biotech, Tutorial Analysis.
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Vertical Integration: Malungtaron nga Sourcing → GMP Extraction → pH-Managed Purification → Lyophilization.
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5. Rigorous Product Specs
Klase sa Kontaminante | Parameter | Espesipikasyon Limitahan | Tan-awa ang Teknik |
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Mga pestisidyo | Mga chlorpyrifos | ≤ 0.01 mg/kg | GC-MS/MS |
Cypermethrin | ≤ 0.05 mg/kg | GC-ECD | |
Whole Different Pesticides | ≤ 0.1 mg/kg (every) | EU 2021/601 | |
Bug-at nga Metal | Pb | ≤ 1.0 mg/kg | ICP-MS (USP <232>) |
Ingon | ≤ 0.5 mg/kg | ICP-MS (USP <232>) | |
Cd | ≤ 0.5 mg/kg | ICP-MS (USP <232>) | |
Hg | ≤ 0.1 mg/kg | CVAAS (USP <232>) | |
Microbiological | TAMC | ≤ 10³ CFU/g | USP <61> |
TYMC | ≤ 10² CFU/g | USP <61> | |
E. coli | Wala sa 10g | USP <62> | |
Salmonella spp. | Absent in 375g | USP <62> | |
Important High quality | Camptothecin Purity | ≥ 99.0% (HPLC) | HPLC-PDA (USP <621>) |
Lactone Kind | ≥ 95.0% | pH-Particular HPLC | |
Water Content | ≤ 2.0% | Karl Fischer (USP <921>) | |
Nabilin nga mga Solvent | Class 1/2 Solvents: Undetected | GC-FID (ICH Q3C) |
6. Superior nga Workflow sa Paggama
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Sustainable Harvesting: Camptotheca acuminata cultivated below GACP tips.
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Pinili nga Pagkuha: Ethanol/Water o Supercritical CO₂ extraction of bark/seeds.
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Panguna nga Pagputli: Liquid-liquid partitioning (CH₂Cl₂/H₂O), adsorbent chromatography (SiO₂, polyamide).
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Lactone Stabilization: pH-controlled crystallization (pH 3.5-4.5) to maximise lactone yield.
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Last Purification: Pangandam nga HPLC (C18 column, MeOH/H₂O/TFA cell section).
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Pagpauga: Lyophilization (-50°C, <10 Pa) to protect lactone ring & stability.
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Paglusad sa QC: Puno Si CoA verifying identification, purity, lactone content material, contaminants.
7. Key Application Areas
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Oncology Medicine: Precursor for Irinotecan (CPT-11), Topotecan, Belotecan.
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Most cancers Analysis: Software compound for DNA harm response, apoptosis, drug resistance research.
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Drug Supply Techniques: Loaded into liposomes, nanoparticles, polymer conjugates to boost solubility/concentrating on.
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Antiviral/Antiparasitic Improvement: Investigational agent for novel therapeutics.
8. cGMP High quality Management Protocol
Si Shaanxi Zhonghong nagtrabaho sa usa ka tiered QC technique:
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Pag-ila: FT-NMR (¹H/¹³C), HPLC-UV/PDA spectral match vs. USP reference customary.
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Assay & Impurities: HPLC-ELSD/PDA quantifies CPT (≥99.0%) and detects ≤0.1% associated compounds (10-deacetylcamptothecin, camptothecin carboxylate).
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Lactone Content: Validated pH-specific RP-HPLC methodology distinguishes lactone/carboxylate types.
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Kontaminante: ICP-MS for heavy metals (USP <232>), GC-MS/MS for 500+ pesticides (EU 2021/601), LC-MS/MS for mycotoxins, USP <61>/<62> for microbiology.
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Kalig-on: Actual-time & accelerated ICH Q1A(R2) research verify 24-month shelf-life at -20°C (desiccated, argon ambiance).
9. Safe Packaging & Logistics
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Major Pack: Amber glass vials sealed below argon, full of desiccant.
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Secondary Pack: Vacuum-sealed aluminum luggage sulod UN-certified HDPE containers.
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Pagtipig: -20°C ± 5°C; defend from gentle/moisture.
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Paghatud: International cold-chain logistics (-15°C to -25°C) by way of DHL FedEx UltraCold.
10. Mechanisms, Functions & Challenges
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Mekanismo: Traps Topo I-DNA cleavable complexes → Collision with replication forks → DSBs → ATR/Chk1 activation → p53-mediated apoptosis.
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Kabag-ohan: ni Zhonghong PEGylated liposomal CPT (Patent: CN202210XXXXXX) enhances tumor concentrating on.
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Mga utlanan sa pag-analisa:
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Novel Analogues: 7-Silylcamptothecins (improved lactone stability).
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Sagol nga Therapies: With PARP inhibitors, immunotherapy.
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Biomarkers: Predictive biomarkers for CPT sensitivity (ERCC1, Topo I ranges).
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Mga hagit: Lactone instability, myelosuppression, ABCG2-mediated drug resistance, tumor heterogeneity.
11. Steadily Requested Questions (FAQ)
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Q1: Can I take Camptothecin as a complement?
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A: Completely NOT. CPT is a potent cytotoxic compound with extreme unintended effects. Use solely below medical supervision in FDA-approved by-product types (e.g., Irinotecan) or for managed analysis.
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Q2: Why is lactone kind important?
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A: Solely the closed lactone ring binds Topo I. The open carboxylate kind is inactive and will trigger renal toxicity. Zhonghong ensures ≥95% lactone content material by way of lyophilization.
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Q3: How does Camptothecin differ from Nattokinase for kidneys?
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A: CPT carries nephrotoxicity dangers (tubular harm). Nattokinase, a fibrinolytic enzyme, lacks strong proof for direct kidney advantages. Neither is nephroprotective.
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This autumn: What analytical strategies verify Zhonghong’s CPT purity?
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A: HPLC-PDA/ELSD (purity), UPLC-QTOF-MS (impurities), FT-NMR (construction), pH-HPLC (lactone quantification), ICP-MS (heavy metals).
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Q5: Do you supply Camptothecin derivatives?
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A: Sure. GMP-grade 10-Hydroxycamptothecin, SN-38 (Irinotecan metabolite), customized synthesis obtainable.
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12. The place to Purchase?
Supply research-grade & GMP Camptothecin:
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E-mail: liaodaohai@gmail.com
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Internet: www.aiherba.com
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hangyo: COA, MSDS, customized synthesis quotes.
13. Panapos
Camptothecin stays a cornerstone of topoisomerase-targeted oncology. Its medical impression by way of semisynthetic derivatives underscores its irreplaceable function. Success hinges on securing ultra-pure, lactone-stabilized materials with verifiable traceability. Shaanxi Zhonghong delivers >99% HPLC purity CPT pinaagi sa patented stabilization expertise, pagsunod sa cGMP, ug unmatched analytical rigor – empowering drug discovery and superior therapeutics.
14. Mga pakisayran
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Wall ME, et al. (1966). J Am Chem Soc. 88:3888–3890. [DOI:10.1021/ja00968a057]
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Hsiang YH, et al. (1985). J Biol Chem. 260:14873–14878. [PMID:2997227]
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Pommier Y. (2006). Nat Rev Most cancers. 6:789–802. [DOI:10.1038/nrc1977]
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USP-NF Monograph: Camptothecin. USP44-NF39.
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ICH Q3C (R8): Residual Solvents. (2021).
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FDA Steerage: Irinotecan Label. (2023).
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Thomas CJ, et al. (2004). J Med Chem. 47:3972–3981. [DOI:10.1021/jm030660+]
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Du W, et al. (2022). Acta Pharm Sin B. 12:3006–3025. [DOI:10.1016/j.apsb.2022.03.011]
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GLS-010-IPHASE Research Protocol (NCT04501563).
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EMA Evaluation Report: Topotecan (2020). EMA/CHMP/89262/2020.
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